Bioactivity | FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor[1]. | ||||||||||||
Target | hFEN1 | ||||||||||||
Invitro | FEN1 inhibition selectively impairs proliferation of colon cancer cells deficient in Cdc4 and Mre11a, both frequently mutated in colorectal cancers. FEN1 has also emerged as a potential chemosensitizing target due to its role in LP-BER since it is critical for repair of Methyl methanesulfonate-induced alkylation damage, and its knockdown or inhibition increases sensitivity to Temozolomide in glioblastoma and colorectal cancer cell lines[1]. | ||||||||||||
Name | FEN1-IN-4 | ||||||||||||
CAS | 1995893-58-7 | ||||||||||||
Formula | C12H12N2O3 | ||||||||||||
Molar Mass | 232.24 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Jack C Exell, et al. Cellularly Active N-hydroxyurea FEN1 Inhibitors Block Substrate Entry to the Active Site. Nat Chem Biol. 2016 Oct;12(10):815-21. |